Thermann M, Lorenz W, Schmal A, Schingale F, Dormann P, Hamelmann H
Agents Actions. 1977 Mar;7(1):97-101. doi: 10.1007/BF01964888.
The effects of the H1-receptor antagonist dimethpyrindene and the H2-receptor antagonist burimamide on circulatory and respiratory parameters and on plasma histamine levels were tested in 21 mongrel dogs. Both drugs released histamine. The incidence for this effect was 10/11 in the case of dimethpyrindene and 5/10 in the case of burimamide. Following dimethpyrindene all animals showed arterial hypotension, pulmonal hypertension, decrease in peripheral resistance and hyperventilation. The portal venous pressure was increased in dogs reacting by a histamine release. Following burimamide both an initial arterial hypertension and a subsequent hypotension were observed the latter being more pronounced in the group with histamine release. In this group the portal venous pressure raised considerably. In the non-reacting animals cardiac output was elevated, probably due to a release of catecholamines. It seemed remarkable that the effect of exogenous histamine on portal venous pressure was completely blocked by dimethpyrindene, but not the action of histamine released by the drug itself. It is concluded that the effects of anti-histaminic drugs on possibly histamine-induced physiological and pathophysiological processes should be interpreted very carefully as far as their specificity is concerned.
在21只杂种犬身上测试了H1受体拮抗剂二甲茚定和H2受体拮抗剂布立马胺对循环和呼吸参数以及血浆组胺水平的影响。两种药物均能释放组胺。二甲茚定出现这种效应的发生率为10/11,布立马胺为5/10。给予二甲茚定后,所有动物均出现动脉低血压、肺动脉高压、外周阻力降低和通气过度。组胺释放反应的犬门静脉压力升高。给予布立马胺后,观察到起初出现动脉高血压,随后出现低血压,后者在组胺释放组中更为明显。在该组中,门静脉压力显著升高。在无反应的动物中,心输出量升高,可能是由于儿茶酚胺释放所致。值得注意的是,外源性组胺对门静脉压力的作用被二甲茚定完全阻断,但药物自身释放的组胺的作用却未被阻断。结论是,就抗组胺药物的特异性而言,其对可能由组胺诱导的生理和病理生理过程的影响应非常谨慎地加以解释。